A-867744

A-867744 is a positive allosteric modulator of α7 nAChRs (IC50 values are 0.98 and 1.12 μM for human and rat α7 receptor ACh-evoked currents respectively, in X. laevis oocytes). Displays no activity at 5-HT3A, α3β4 or α4β2 nAChRs.IC50 value: ~ 1 uMTarget: α7 nAChRTarget:

Signaling Pathways >> Autophagy >> Autophagy

Signaling Pathways >> Membrane Transporter/Ion Channel >> nAChR

Signaling Pathways >> Neuronal Signaling >> nAChR

Research Areas >> Neurological Disease

[1]. Faghih R, et al. Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor.J Med Chem. 2009 May 28;52(10):3377-84.

[2]. Malysz J, et al. In vitro pharmacological characterization of a novel allosteric modulator of alpha 7 neuronal acetylcholine receptor, 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744), exhibiting unique pharmacological profile.J Pharmacol Exp Ther. 2009 Jul;330(1):257-67. Epub 2009 Apr 23.

[3]. Malysz J, et al. In vitro pharmacological characterization of a novel selective alpha7 neuronal nicotinic acetylcholine receptor agonist ABT-107.J Pharmacol Exp Ther. 2010 Sep 1;334(3):863-74. Epub 2010 May 26.

[4]. Hu M, et al. Positive allosteric modulation of alpha7 neuronal nicotinic acetylcholine receptors: lack of cytotoxicity in PC12 cells and rat primary cortical neurons.Br J Pharmacol. 2009 Dec;158(8):1857-64.

[5]. Ramin Faghih, et al. Discovery of 4-(5-(4-Chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a Novel Positive Allosteric Modulator of the α7 Nicotinic Acetylcholine Receptor J. Med. Chem., 2009, 52 (10), pp 3377-3384

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